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    Substituted fused tricyclic compounds, compositions and medicinal applications thereof
    1.
    发明授权
    Substituted fused tricyclic compounds, compositions and medicinal applications thereof 有权
    取代的稠合三环化合物，组合物及其药用应用

    公开(公告)号：US09115133B2

    公开(公告)日：2015-08-25

    申请号：US14006630

    申请日：2012-03-21

    申请人： Dinesh Barawkar ,  Tanushree Bende ,  Robert Zahler ,  Anish Bandyopadhyay ,  Robindro Singh Sarangthem ,  Jignesh Doshi ,  Yogesh Waman ,  Rushikesh Jadhav ,  Umesh Prasad Singh

    发明人： Dinesh Barawkar ,  Tanushree Bende ,  Robert Zahler ,  Anish Bandyopadhyay ,  Robindro Singh Sarangthem ,  Jignesh Doshi ,  Yogesh Waman ,  Rushikesh Jadhav ,  Umesh Prasad Singh

    IPC分类号： C07D471/14 ,  A61K31/4375 ,  A61K31/5025 ,  A61K31/5377 ,  A61K31/519 ,  A61K45/06 ,  A61K31/496

    CPC分类号： C07D471/14 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  Y02A50/475 ,  A61K2300/00

    摘要： The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity. Such conditions include, but not limited to, arthritis, Alzheimer's disease, autoimmune thyroid disorders, cancer, diabetes, leukemia, T-cell prolymphocytic leukemia, lymphoma, myleoproliferation disorders, lupus, multiple myeloma, multiple sclerosis, osteoarthritis, sepsis, psoriatic arthritis, prostate cancer, T-cell autoimmune disease, inflammatory diseases, chronic and acute allograft transplant rejection, bone marrow transplant, stroke, asthma, chronic obstructive pulmonary disease, allergy, bronchitis, viral diseases, or Type I diabetes, complications from diabetes, rheumatoid arthritis, asthma, Crohn's disease, dry eye, uveitis, inflammatory bowel disease, organ transplant rejection, psoriasis and ulcerative colitis. The present disclosure also relates to process for the preparation of such compounds, and to pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及式（I）或（Ia）的取代的稠合三环化合物，其互变异构体，多晶型物，立体异构体，前药，溶剂合物，共晶体，药学上可接受的盐，含有它们的药物组合物和治疗病症和疾病的方法 由JAK活动介导。 本发明的化合物可用于治疗，预防或抑制由JAK活性介导的疾病和病症。 这些病症包括但不限于关节炎，阿尔茨海默氏病，自身免疫性甲状腺疾病，癌症，糖尿病，白血病，T细胞淋巴细胞性白血病，淋巴瘤，组织增生障碍，狼疮，多发性骨髓瘤，多发性硬化，骨关节炎，败血症，牛皮癣关节炎， 前列腺癌，T细胞自身免疫疾病，炎性疾病，慢性和急性同种异体移植排斥反应，骨髓移植，中风，哮喘，慢性阻塞性肺病，过敏，支气管炎，病毒性疾病或I型糖尿病，糖尿病并发症，类风湿关节炎 ，哮喘，克罗恩病，干眼症，葡萄膜炎，炎性肠病，器官移植排斥反应，牛皮癣和溃疡性结肠炎。 本公开还涉及制备这些化合物的方法以及含有它们的药物组合物。

    SUBSTITUTED FUSED TRICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF
    2.
    发明申请
    SUBSTITUTED FUSED TRICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF 有权
    取代的熔融三氯化合物，其组合物和药物应用

    公开(公告)号：US20140023614A1

    公开(公告)日：2014-01-23

    申请号：US14006630

    申请日：2012-03-21

    申请人： Dinesh Barawkar ,  Tanushree Bende ,  Robert Zahler ,  Anish Bandyopadhyay ,  Robindro Singh Sarangthem ,  Jignesh Doshi ,  Yogesh Waman ,  Rushikesh Jadhav ,  Umesh Prasad Singh

    发明人： Dinesh Barawkar ,  Tanushree Bende ,  Robert Zahler ,  Anish Bandyopadhyay ,  Robindro Singh Sarangthem ,  Jignesh Doshi ,  Yogesh Waman ,  Rushikesh Jadhav ,  Umesh Prasad Singh

    IPC分类号： C07D471/14 ,  A61K31/5025 ,  A61K45/06 ,  A61K31/519 ,  A61K31/4375 ,  A61K31/5377 ,  A61K31/496

    CPC分类号： C07D471/14 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  Y02A50/475 ,  A61K2300/00

    摘要： The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity. Such conditions include, but not limited to, arthritis, Alzheimer's disease, autoimmune thyroid disorders, cancer, diabetes, leukemia, T-cell prolymphocytic leukemia, lymphoma, myleoproliferation disorders, lupus, multiple myeloma, multiple sclerosis, osteoarthritis, sepsis, psoriatic arthritis, prostate cancer, T-cell autoimmune disease, inflammatory diseases, chronic and acute allograft transplant rejection, bone marrow transplant, stroke, asthma, chronic obstructive pulmonary disease, allergy, bronchitis, viral diseases, or Type I diabetes, complications from diabetes, rheumatoid arthritis, asthma, Crohn's disease, dry eye, uveitis, inflammatory bowel disease, organ transplant rejection, psoriasis and ulcerative colitis. The present disclosure also relates to process for the preparation of such compounds, and to pharmaceutical compositions containing them.

    摘要翻译： 本发明涉及式（I）或（Ia）的取代的稠合三环化合物，其互变异构体，多晶型物，立体异构体，前药，溶剂合物，共晶体，药学上可接受的盐，含有它们的药物组合物和治疗病症和疾病的方法 由JAK活动介导。 本发明的化合物可用于治疗，预防或抑制由JAK活性介导的疾病和病症。 这些病症包括但不限于关节炎，阿尔茨海默氏病，自身免疫性甲状腺疾病，癌症，糖尿病，白血病，T细胞淋巴细胞性白血病，淋巴瘤，组织增生障碍，狼疮，多发性骨髓瘤，多发性硬化，骨关节炎，败血症，牛皮癣关节炎， 前列腺癌，T细胞自身免疫疾病，炎性疾病，慢性和急性同种异体移植排斥反应，骨髓移植，中风，哮喘，慢性阻塞性肺病，过敏，支气管炎，病毒性疾病或I型糖尿病，糖尿病并发症，类风湿关节炎 ，哮喘，克罗恩病，干眼症，葡萄膜炎，炎性肠病，器官移植排斥反应，牛皮癣和溃疡性结肠炎。 本公开还涉及制备这些化合物的方法以及含有它们的药物组合物。